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Catalog No.
Product Name
Application
Product Information
Citations
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Endothelin receptor antagonist
Macitentan is an orally active, non-peptide dual endothelin ETA and ETB receptor antagonist for the potential treatment of idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH). -
EP4 antagonist
MK-2894 sodium salt is a highly potent and selective second generation EP4 antagonist. -
CaSR antagonist
NPS-2143 hydrochloride (SB-262470A hydrochloride), an orally active calcilytic agent, is a selective and potent calcium ion-sensing receptor (CaSR) antagonist. -
EP4 antagonist
ONO-AE3-208 is an EP4 antagonist, and suppresses cell invasion, migration, and metastasis of prostate cancer. -
A2a receptor antagonist
SYN115 is an orally administered, potent and selective inhibitor of the adenosine 2a (A2a) receptor that is being developed initially for the treatment of Parkinson?€?s disease, but may also have utility in other CNS disorders. -
ETA receptor antagonist
Sitaxentan sodium (TBC-11251) is a selective endothelin receptor-A antagonist with IC50 and Ki of 1.4 nM and 0.43 nM, respectively. -
ETA receptor antagonist
Sitaxsentan (IPI 1040; TBC-11251) is a selective endothelin A (ETA) receptor antagonist. Antihypertensive. Sitaxsentan is used in treatment of chronic heart failure. -
5-HT6 receptor antagonist
SB271046 Hydrochloride is a potent, selective and orally active 5-HT6 receptor antagonist with pKi of 8.9. -
LTD4 receptor antagonist
Verlukast (MK-0679) is a potent leukotriene D4 antagonist -
histamine receptor antagonist
Cyproheptadine hydrochloride is a histamine receptor antagonist for 5-HT2 receptor with IC50 of 0.6 nM. -
NMDA receptor antagonist
Orphenadrine citrate is a NMDA receptor antagonist with Ki of 6.0 +/- 0.7 μM, HERG potassium channel blocker. -
H2 receptor antagonist
Lafutidine is a second generation H2 receptor antagonist having multimodal mechanism of action. -
5-HT antagonist
Tegaserod functions as a motility stimulant, achieving its desired therapeutic effects through activation of the 5-HT4 receptors of the enteric nervous system in the gastrointestinal tract. It also stimulates gastrointestinal motility and the peristaltic reflex, and allegedly reduces abdominal pain. Additionally, tegaserod is a 5-HT2B receptor antagonist. -
neurokinin-1 receptor antagonist
Fosaprepitant (MK-0517, L-758,298) is a water-soluble phosphoryl prodrug for Aprepitant which is a NK1 antagonist. -
Prostaglandin D2 receptor CRTH2 antagonist
CAY10471 Racemate (TM30089 Racemate) is a potent and highly selective prostaglandin D2 receptor CRTH2 antagonist. -
CCK-A receptor antagonist
Loxiglumide (CR1505) is a cholecystokinin antagonist -
NT Antagonist
SR 48692 represents a new, potent, nonpeptide antagonist radioligand of the NT receptor that differentiates between agonist- and antagonist-receptor interactions. -
D2/5-HT2 receptor antagonist
Blonanserin is a D2/5-HT2 receptor antagonist; atypical antipsychotic. -
Leukotriene receptor antagonist
Pranlukast is a selective cysteinyl leukotriene receptor antagonist. -
CB1 antagonist
CP 945598 is a potent and highly selective CB1 antagonist. -
CRTH2 antagonist
OC 000459 is a potent, oral and selective CRTH2 (also known as DP2) antagonist. -
AR antagonist
Diprophylline is a xanthine derivative with bronchodilator and vasodilator effects. -
PAR4 antagonist
BMS-986120 is a first-in-class oral and reversible protease-activated receptor 4 (PAR4) antagonist, with IC50s of 9.5 nM and 2.1 nM in human and monkey blood, respectively. -
PAF antagonist
Aglafoline is an effective PAF antagonist not only in vitro, but also in vivo. -
5-HT4 receptor antagonist
5-HT4 antagonist 1 is a 5-HT4 receptor antagonist with a pKi of 9.6. -
5-HT2A receptor antagonist
Lumateperone Tosylate is a 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a SERT blocker (Ki = 61 nM). -
MCH-1 antagonist
MCH-1 antagonist 1 is a potent melanin concentrating hormone (MCH-1) antagonist with a Ki of 2.6 nM. MCH-1 antagonist 1 also inhibits CYP3A4 with an IC50 of 10 μM. -
combined Ca2+/5-HT2 antagonist
Nexopamil racemate is the racemate of Nexopamil. Nexopamil is a combined Ca2+/5-HT2 antagonist on thrombus formation in vivo and on platelet aggregation in vitro. -
5-HT2 receptor antagonist
Methiothepin mesylate is a potent and non-selective 5-HT2 receptor antagonist, with pKds of 7.10 (5-HT1A), 7.28 (5HT1B), 7.56 (5HT1C), 6.99 (5HT1D), 7.0 (5-HT5A), 7.8 (5-HT5B), 8.74 (5-HT6), and 8.99 (5-HT7), and pKis of 8.50 (5HT2A), 8.68 (5HT2B), and 8.35 (5HT2C). -
adenosine A3 receptor antagonist
MRE3008F20 is a highly potent and selective antagonist of adenosine A3 receptor (AA3R), inhibits agonist-induced cAMP elevation in resting T lymphocytes with an IC50 of 5 nM. -
histamine H1 receptor antagonist
ReN 1869 hydrochloride is a novel, selective histamine H1 receptor antagonist, which demonstrates affinity to the histamine H1 receptor (guinea pig brain) with Ki of 0.19±0.04 μM and the non-selective ?? site (guinea pig brain) with Ki of 0.45 μM. -
PGF2α receptor antagonist
OBE022 is an oral and selective prostaglandin F2α (PGF2α) receptor antagonist, with Kis of 1 nM, 26 nM for human and rat FP receptors, respectively. -
H4R antagonist
H4R antagonist 1 is a potent and highly selective histamine H4 receptor (H4R) antagonist with an IC50 of 27 nM. -
CRTh2 antagonist
CRTh2 antagonist 1 is a CRTh2 antagonist with an IC50 of 89 nM.
